Ispitivanje utjecaja pomoćnih tvari na fizičku stabilnost suspenzije posakonazola

master's thesis

• Title (english): Investigation of the influence of excipients on the stability of the posaconazole suspension
• Author: Jelena Orešković
• Mentor: Biserka Cetina Čižmek (mentor)
• Committee member: Biserka Cetina Čižmek
• Committee member: Jelena Filipović-Grčić
• Committee member: Ivan Pepić
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; Zagreb
• Defense date and country: 2015-06-12, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

U okviru ovog diplomskog rada provedena je morfološka karakterizacija čestica uzoraka posakonazola sljedećim tehnikama: optičkom mikroskopijom, pretražnom elektronskom mikroskopijom, laserskom difrakcijom svjetlosti pri niskom kutu i dinamičkim svjetlosnim raspršenjem.
Pripremanjem suspenzija posakonazola s jednom od površinski-aktivnih tvari (natrijevim dodecilsulfatom, cetiltrimetilamonijevim bromidom, polisorbatom 80 i polioksietilen lauril-eterom) ili s jednim od polimernih stabilizatora (poloksamerom 407 i hidroksipropil celulozom) utvrđen je njihov utjecaj na stabilizaciju suspenzije. Potom su izrađene suspenzije s omjerima koncentracija aktivne i pomoćne tvari 10:1 i 100:1 te je izmjeren zeta-potencijal, provedena je mikroskopska analiza, promatran je izgled suspenzija i resuspenzibilnost. Stoga su izrađene suspenzije posakonazola s kombinacijama jedne površinski-aktivne tvari i jednog polimera u omjeru 100:1:1 te su i njima utvrđena sva navedena svojstva.
Paralelno s ispitivanjem svojstava suspenzija određen je kut močenja na komprimatima posakonazola. Kut močenja određen je za vodu i sve pojedinačne pomoćne tvari te za kombinacije oba polimera sa svim ispitanim površinski-aktivnim tvarima.
Suspenzija posakonazola s hidroksipropil celulozom i natrijevim dodecilsulfatom je suspenzija s najpovoljnijim svojstvima: s najvećim zeta-potencijalom, bez aglomerata te s kratkim vremenom resuspenzibilnosti. Uz to, kombinacija tih dviju pomoćnih tvari daje najniži kut močenja. Stoga tako pripremljena suspenzija može poslužiti kao prijedlog za daljnji razvoj formulacije gotovog proizvoda.

Abstract (english)

In this thesis morphological characterization of samples of posaconazole was carried out with the following techniques: optical microscopy, scanning electron microscopy, low-angle laser light scattering and dynamic light scattering.
By preparing suspensions of posaconazole with one of the surface-active agents (sodium dodecyl sulfate, cetyltrimethylammonium bromide, polysorbate 80 and polyoxyethylene lauryl ether) either with one of the polymeric stabilizer (poloxamer 407 and hydroxypropyl cellulose), their effect on the stabilization of the suspension was determined. Suspensions were made in the concentration ratios of the active and auxiliary substances 10:1 as well as 100:1. Suspensions were characterized by means of zeta potential determination, optical microscopy, appearance and resuspensibility observation. Afterwards posaconazole suspensions with the combination of one surfactant and the polymer in a ratio of 100:1:1 were prepared and characterized.
Parallel with the examination of the properties of the suspensions, the contact angle of posaconazole comprimates was mesured. The contact angle was determined for water and all of the individual excipients and combinations of both polymers with the tested surfactants.
The posaconazole suspension with hydroxypropyl cellulose and sodium dodecyl sulfate is a suspension with optimal properties: the highest zeta potential, no agglomerates and short time of resuspensibility. Besides it is the combination of two excipients that has the lowest contact angle. Therefore this suspension could be proposed for development of final drug product.

• Keywords: posakonazol; suspenzija; stabilnost
• Keywords (english): posaconazole; suspension; stability
• Language: croatian
• URN:NBN: urn:nbn:hr:163:026216
• Study programme: Title: Pharmacy; Study programme type: university; Study level: integrated undergraduate and graduate; Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2016-01-18 11:40:04